114289-47-3
Chemical Structure
PD 128042
Synonym(s): CI 976
- CAS No.: 114289-47-3
- Formula:C23H39NO4
- Molecular Weight:393.56
IUPAC Name: 2,2-dimethyl-N-(2,4,6-trimethoxyphenyl)dodecanamide
InChIKey: WAFNZAURAWBNDZ-UHFFFAOYSA-N
SMILES: CCCCCCCCCCC(C)(C)C(NC1=C(C=C(OC)C=C1OC)OC)=O
Biological Activity: PD 128042 (CI 976) is a potent, orally active, and selective inhibitor of ACAT (acyl coenzyme A:cholesterol acyltransferase) with an IC50s of 73 nM. PD 128042 is also a potent LPAT (lysophospholipid acyltransferase) inhibitor. PD 128042 inhibits Golgi-associated LPAT activity (IC50=15 μM). PD 128042 inhibits multiple membrane trafficking steps, including ones found in the endocytic and secretory pathway[1][2][3].
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PD 128042 | 99.97% | PD 128042 (CI 976) is a potent, orally active, and selective inhibitor of ACAT (acyl coenzyme A:cholesterol acyltransferase) with an IC50s of 73 nM. PD 128042 is also a potent LPAT (lysophospholipid acyltransferase) inhibitor. PD 128042 inhibits Golgi-associated LPAT activity (IC50=15 μM). PD 128042 inhibits multiple membrane trafficking steps, including ones found in the endocytic and secretory pathway. | ||||||||||||||||||||
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PD 128042 (Standard) | ≥98% | PD 128042 (Standard) is the analytical standard of PD 128042. This product is intended for research and analytical applications. PD 128042 (CI 976) is a potent, orally active, and selective inhibitor of ACAT (acyl coenzyme A:cholesterol acyltransferase) with an IC50s of 73 nM. PD 128042 is also a potent LPAT (lysophospholipid acyltransferase) inhibitor. PD 128042 inhibits Golgi-associated LPAT activity (IC50=15 μM). PD 128042 inhibits multiple membrane trafficking steps, including ones found in the endocytic and secretory pathway. | ||||||||||||||||||||
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References
- [1]. Chambers K, et al. A unique lysophospholipid acyltransferase (LPAT) antagonist, CI-976, affects secretory and endocytic membrane trafficking pathways. J Cell Sci. 2005;118(Pt 14):3061-3071. [Content Brief]
- [2]. O'Brien PM, et al. Inhibitors of acyl-CoA:cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 8. Incorporation of amide or amine functionalities into a series of disubstituted ureas and carbamates. Effects on ACAT inhibition in vitro and efficacy in vivo. J Med Chem. 1994;37(12):1810-1822. [Content Brief]
- [3]. Drecktrah D, et al. Inhibition of a Golgi complex lysophospholipid acyltransferase induces membrane tubule formation and retrograde trafficking. Mol Biol Cell. 2003;14(8):3459-3469. [Content Brief]
